缺氧诱导因子1（HIF-1）有两个亚基，在缺氧情况下，HIF-1α会过度表达，HIF-1α转录活性的增加与肿瘤进展、血管生成、转移和侵袭密切相关。
近日European Journal of Pharmacology杂志上的一则研究证实天然化合物补骨脂二氢黄酮甲醚 Bavachinin在体外和体内有较强的抗血管生成活性。Bavachinin浓度依赖性抑制人KB癌（HeLa细胞的衍生细胞株）HIF-1α活性，其机制是通过促进（VHL）与HIF-1α之间的相互作用。
此外，Bavachinin降低与血管生成和能量代谢相关基因的表达如血管内皮生长因子（VEGF）、Glut1和己糖激酶2。Bavachinin也抑制人类脐静脉内皮细胞（内皮细胞）的管腔形成以及KB细胞在体外的迁移能力。体内研究显示，给予KB移植瘤裸鼠每周三次注射Bavachinin，共持续四星期能显著减少肿瘤体积和CD31的表达。这些数据表明Bavachinin可以作为抑制肿瘤血管生成的治疗剂。（生物谷：Bioon.com）
doi:10.1016/j.ejphar.2012.06.028
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Anti-angiogenic and anti-tumor activity of Bavachinin by targeting hypoxia-inducible factor-1α
Manoj Nepala, b, Hwa Jung Choia, Bo-Yun Choia, b, Se Lim Kima, Jae-Ha Ryuc, Ho Hee Kimc, Young-Hoon Leed, Yunjo Soha,
Hypoxia-inducible factor-1 (HIF-1) consists of two subunits, the HIF-1β, which is constitutively expressed, and HIF-1α, which is oxygen-responsive. HIF-1α is over-expressed in response to hypoxia, increasing transcriptional activity linked to tumor progression, angiogenesis, metastasis, and invasion. This study aimed to demonstrate that the natural compound, Bavachinin, has potent anti-angiogenic activity in vitro and in vivo. Bavachinin inhibited increases in HIF-1α activity in human KB carcinoma (HeLa cell derivative) and human HOS osteosarcoma cells under hypoxia in a concentration-dependent manner, probably by enhancing the interaction between von Hippel–Lindau (VHL) and HIF-1α. Furthermore, Bavachinin decreased transcription of genes associated with angiogenesis and energy metabolism that are regulated by HIF-1, such as vascular endothelial growth factors (VEGF), Glut 1 and Hexokinase 2. Bavachinin also inhibited tube formation in human umbilical vein endothelial cells (HUVECs) as well as in vitro migration of KB cells. In vivo studies showed that injecting Bavachinin thrice weekly for four weeks significantly reduced tumor volume and CD31 expression in nude mice with KB xenografts. These data indicate that Bavachinin could be used as a therapeutic agent for inhibiting tumor angiogenesis.
